bs-60178C

DATASHEET

Formulation Powder

Storage: Store in dry, dark place at -20C for 1 year.

Product Information:

Molecular Weight: 296.32

Formula: C17 H16 N2 O3

CAS Number: 950762-95-5

InChi Key: AJRGHIGYPXNABY-UHFFFAOYSA-N

InChi: InChI=1S/C17H16N2O3/c1-22-15-6-2-12(3-7-15)11-19-9-8-13-4-5-14(10-16(13)19)17(20)18-21/h2-10,21H,11H2,1H3,(H,18,20)

Smiles: COC1C=CC(CN2C=CC3=CC=C(C=C23)C(=O)NO)=CC=1

Purity: 98.0

Solubility: DMSO up to 100 mM

Appearance: Solid Power.

Shelf Life: 1.0 years

Description:

PCI-34051 is a potent and selective inhibitor of histone deacetylase 8 (HDAC8) with an IC50 ~10 nM. It displays >200 fold selectivity over other HDAC isoforms 1, 2, 3, 6 and 10. PCI-34051 has a unique mechanism of action involving PLCgamma1 activation and calcium-induced apoptosis, and could offer benefits including a greater therapeutic index for treating T-cell malignancies. PCI-34051 induces caspase-dependent apoptosis in cell lines derived from T-cell lymphomas or leukemia, but not in other hematopoietic or solid tumor lines. Unlike broad-spectrum HDAC inhibitors, PCI-34051 does not cause detectable histone or tubulin acetylation. Cells defective in T-cell receptor signaling were still sensitive to PCI-34051-induced apoptosis, whereas a phospholipase C-gamma1 (PLCgamma1)-defective line was resistant. In addition, steady-state calcium levels strongly influence the apoptosis induced by PCI-34051. It also induces cytochrome c release from mitochondria.